ECSP055768A - CONDENSED AZOL-PYRIMIDINE DERIVATIVES - Google Patents
CONDENSED AZOL-PYRIMIDINE DERIVATIVESInfo
- Publication number
- ECSP055768A ECSP055768A EC2005005768A ECSP055768A ECSP055768A EC SP055768 A ECSP055768 A EC SP055768A EC 2005005768 A EC2005005768 A EC 2005005768A EC SP055768 A ECSP055768 A EC SP055768A EC SP055768 A ECSP055768 A EC SP055768A
- Authority
- EC
- Ecuador
- Prior art keywords
- pi3k
- diseases
- disease
- present
- derivatives
- Prior art date
Links
- DDWJFSYHYPDQEL-UHFFFAOYSA-N pyrimidine;1h-pyrrole Chemical class C=1C=CNC=1.C1=CN=CN=C1 DDWJFSYHYPDQEL-UHFFFAOYSA-N 0.000 title 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 5
- 108091007960 PI3Ks Proteins 0.000 abstract 4
- 102000003993 Phosphatidylinositol 3-kinases Human genes 0.000 abstract 4
- 108090000430 Phosphatidylinositol 3-kinases Proteins 0.000 abstract 4
- 201000010099 disease Diseases 0.000 abstract 3
- 230000000694 effects Effects 0.000 abstract 3
- 208000035475 disorder Diseases 0.000 abstract 2
- 230000005764 inhibitory process Effects 0.000 abstract 2
- 208000028867 ischemia Diseases 0.000 abstract 2
- 238000011321 prophylaxis Methods 0.000 abstract 2
- 238000011282 treatment Methods 0.000 abstract 2
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 201000001320 Atherosclerosis Diseases 0.000 abstract 1
- 208000023328 Basedow disease Diseases 0.000 abstract 1
- 206010007572 Cardiac hypertrophy Diseases 0.000 abstract 1
- 208000006029 Cardiomegaly Diseases 0.000 abstract 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 abstract 1
- 206010012438 Dermatitis atopic Diseases 0.000 abstract 1
- 208000005189 Embolism Diseases 0.000 abstract 1
- 208000015023 Graves' disease Diseases 0.000 abstract 1
- 206010019280 Heart failures Diseases 0.000 abstract 1
- 208000012659 Joint disease Diseases 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 208000018737 Parkinson disease Diseases 0.000 abstract 1
- KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical class C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 abstract 1
- 208000001647 Renal Insufficiency Diseases 0.000 abstract 1
- 206010040070 Septic Shock Diseases 0.000 abstract 1
- 208000001435 Thromboembolism Diseases 0.000 abstract 1
- 208000026935 allergic disease Diseases 0.000 abstract 1
- 208000006673 asthma Diseases 0.000 abstract 1
- 201000008937 atopic dermatitis Diseases 0.000 abstract 1
- 230000001363 autoimmune Effects 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 206010012601 diabetes mellitus Diseases 0.000 abstract 1
- 230000004957 immunoregulator effect Effects 0.000 abstract 1
- 230000002757 inflammatory effect Effects 0.000 abstract 1
- 201000006370 kidney failure Diseases 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 230000002107 myocardial effect Effects 0.000 abstract 1
- 208000015122 neurodegenerative disease Diseases 0.000 abstract 1
- 230000007170 pathology Effects 0.000 abstract 1
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 1
- 238000002360 preparation method Methods 0.000 abstract 1
- 208000002815 pulmonary hypertension Diseases 0.000 abstract 1
- 206010039073 rheumatoid arthritis Diseases 0.000 abstract 1
- 206010039083 rhinitis Diseases 0.000 abstract 1
- 230000036303 septic shock Effects 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
- C07D471/14—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/02—Nasal agents, e.g. decongestants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Immunology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pulmonology (AREA)
- Diabetes (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Rheumatology (AREA)
- Hospice & Palliative Care (AREA)
- Endocrinology (AREA)
- Urology & Nephrology (AREA)
- Psychiatry (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Emergency Medicine (AREA)
- Vascular Medicine (AREA)
- Pain & Pain Management (AREA)
- Otolaryngology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
La presente invención se refiere a nuevos derivados de azolpirimidina condensados, a procedimientos para su preparación y a preparaciones farmacéuticas que los contienen. Los derivados de azolpirimidina condensados de la presente invención presentan una mayor potencia para la inhibición de la fosfatidilinositol-3-quinasa (PI3K), especialmente para la inhibición de la PI3K-? y pueden usarse para la profilaxis y tratamiento de enfermedades asociadas con la actividad de PI3K y particularmente con la actividad de PI3K-?. Más específicamente, los derivados de azol de la presente invención son útiles para el tratamiento y profilaxis de las siguientes enfermedades: trastornos inflamatorios e inmunorreguladores tales como asma, dermatitis atópica, rinitis, enfermedades alérgicas, enfermedad pulmonar obstructiva crónica (COPD), choque séptico, enfermedades de las articulaciones, patologías autoinmunes tales como artritis reumatoide, y enfermedad de Graves, cáncer, trastornos de contractilidad del miocardio, insuficiencia cardíaca, tromboembolia, isquemia y aterosclerosis. Los compuestos de la presente invención también son útiles para la hipertensión pulmonar, insuficiencia renal, hipertrofia cardíaca así como trastornos neurodegenerativos tales como enfermedad de Parkinson, enfermedad de Alzheimer, diabetes e isquemia focal, ya que las enfermedades también están relacionadas con la actividad de PI3K en un ser humano o animal.The present invention relates to new condensed azolpyrimidine derivatives, processes for their preparation and pharmaceutical preparations containing them. The condensed azolpyrimidine derivatives of the present invention have a greater potency for the inhibition of phosphatidylinositol-3-kinase (PI3K), especially for the inhibition of PI3K-? and can they be used for the prophylaxis and treatment of diseases associated with the activity of PI3K and particularly with the activity of PI3K- ?. More specifically, the azol derivatives of the present invention are useful for the treatment and prophylaxis of the following diseases: inflammatory and immunoregulatory disorders such as asthma, atopic dermatitis, rhinitis, allergic diseases, chronic obstructive pulmonary disease (COPD), septic shock, joint diseases, autoimmune pathologies such as rheumatoid arthritis, and Graves' disease, cancer, myocardial contractility disorders, heart failure, thromboembolism, ischemia and atherosclerosis. The compounds of the present invention are also useful for pulmonary hypertension, renal failure, cardiac hypertrophy as well as neurodegenerative disorders such as Parkinson's disease, Alzheimer's disease, diabetes and focal ischemia, since the diseases are also related to PI3K activity. In a human or animal being.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP02021861 | 2002-09-30 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ECSP055768A true ECSP055768A (en) | 2005-08-11 |
Family
ID=32039115
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EC2005005768A ECSP055768A (en) | 2002-09-30 | 2005-04-28 | CONDENSED AZOL-PYRIMIDINE DERIVATIVES |
| EC2011005768A ECSP11005768A (en) | 2002-09-30 | 2011-02-07 | CONDENSED AZOL-PYRIMIDINE DERIVATIVES |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EC2011005768A ECSP11005768A (en) | 2002-09-30 | 2011-02-07 | CONDENSED AZOL-PYRIMIDINE DERIVATIVES |
Country Status (32)
| Country | Link |
|---|---|
| US (2) | US7511041B2 (en) |
| EP (2) | EP2042504B1 (en) |
| JP (1) | JP4790266B2 (en) |
| KR (1) | KR101059652B1 (en) |
| CN (1) | CN100384846C (en) |
| AR (2) | AR041426A1 (en) |
| AT (2) | ATE511510T1 (en) |
| AU (1) | AU2003293310B2 (en) |
| BR (1) | BRPI0314830B8 (en) |
| CA (1) | CA2499134C (en) |
| CY (2) | CY1109790T1 (en) |
| DE (1) | DE60324296D1 (en) |
| DK (2) | DK1549652T3 (en) |
| EC (2) | ECSP055768A (en) |
| ES (2) | ES2312843T3 (en) |
| HR (2) | HRP20131159B1 (en) |
| IL (1) | IL166855A (en) |
| MA (1) | MA27483A1 (en) |
| MX (1) | MXPA05001808A (en) |
| MY (1) | MY140756A (en) |
| NO (1) | NO331457B1 (en) |
| NZ (1) | NZ539062A (en) |
| PE (1) | PE20050089A1 (en) |
| PL (1) | PL226562B1 (en) |
| PT (2) | PT1549652E (en) |
| RU (1) | RU2326881C9 (en) |
| SI (2) | SI1549652T1 (en) |
| TW (1) | TWI327570B (en) |
| UA (1) | UA82205C2 (en) |
| UY (1) | UY28001A1 (en) |
| WO (1) | WO2004029055A1 (en) |
| ZA (1) | ZA200503306B (en) |
Families Citing this family (87)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6667300B2 (en) | 2000-04-25 | 2003-12-23 | Icos Corporation | Inhibitors of human phosphatidylinositol 3-kinase delta |
| KR100891599B1 (en) | 2003-08-29 | 2009-04-08 | 미쓰이 가가쿠 가부시키가이샤 | Insecticide for agricultural or horticultural use and method of use thereof |
| LT1761540T (en) | 2004-05-13 | 2017-02-27 | Icos Corporation | Quinazolinones as inhibitors of human phosphatidylinositol 3-kinase delta |
| RU2403258C2 (en) | 2004-10-07 | 2010-11-10 | Бёрингер Ингельхайм Интернациональ Гмбх | Thiazolyldihydroindazoles |
| WO2006040645A1 (en) * | 2004-10-11 | 2006-04-20 | Ranbaxy Laboratories Limited | N-(3,5-dichloropyridin-4-yl)-2,4,5-alkoxy and 2,3,4-alkoxy benzamide derivatives as pde-iv (phophodiesterase type-iv) inhibitors for the treatment of inflammatory diseases such as asthma |
| JP2008537120A (en) | 2005-04-14 | 2008-09-11 | ザ トラスティーズ オブ ボストン ユニバーシティ | Diagnosis of lung injury using classification prediction |
| UA97348C2 (en) * | 2005-07-29 | 2012-02-10 | 4Сц Аг | HETEROCYCLIC NF-kB INHIBITORS |
| WO2007103541A2 (en) | 2006-03-09 | 2007-09-13 | The Trustees Of Boston University | Diagnostic and prognostic methods for lung disorders using gene expression profiles from nose epithelial cells |
| US7517995B2 (en) | 2006-04-06 | 2009-04-14 | Boehringer Ingelheim International Gmbh | Thiazolyl-dihydro-cyclopentapyrazole |
| US7691868B2 (en) | 2006-04-06 | 2010-04-06 | Boehringer Ingelheim International Gmbh | Thiazolyl-dihydro-quinazoline |
| AU2007243457B2 (en) * | 2006-04-26 | 2012-02-23 | F. Hoffmann-La Roche Ag | Pharmaceutical compounds |
| WO2008064244A2 (en) * | 2006-11-20 | 2008-05-29 | The Trustees Of Columbia University In The City Of New York | Phosphoinositide modulation for the treatment of neurodegenerative diseases |
| AR064106A1 (en) * | 2006-12-05 | 2009-03-11 | Bayer Schering Pharma Ag | DERIVATIVES OF 2,3-DIHYDROIMIDAZO [1,2-C] SUBSTITUTED QUINAZOLINE USEFUL FOR THE TREATMENT OF HYPER-PROLIFERATIVE DISEASES ASSOCIATED WITH ANGIOGENESIS |
| EP1953163A1 (en) | 2007-02-01 | 2008-08-06 | Boehringer Ingelheim Pharma GmbH & Co. KG | Pteridinone derivatives as PI3-kinases inhibitors |
| WO2008148023A2 (en) * | 2007-05-23 | 2008-12-04 | Medical College Of Georgia Research Institute, Inc. | Compositions and methods for treating neurological disorders |
| US20100204222A1 (en) * | 2007-09-17 | 2010-08-12 | GlaxoSmithKline, LLC | Pyridopyrimidine derivatives as p13 kinase inhibitors |
| CA2700200A1 (en) | 2007-09-19 | 2009-03-26 | The Trustees Of Boston University | Identification of novel pathways for drug development for lung disease |
| US8859572B2 (en) * | 2008-01-14 | 2014-10-14 | Bayer Intellectual Property Gmbh | Sulfone substituted 2,3-dihydroimidazo [1,2-C] quinazoline derivatives useful for treating hyper-proliferative disorders and diseases with angiogenesis |
| EP2250160B1 (en) | 2008-01-25 | 2015-11-11 | Millennium Pharmaceuticals, Inc. | Thiophenes and their use as phosphatidylinositol 3-kinase (pi3k) inhibitors |
| WO2009111547A1 (en) * | 2008-03-04 | 2009-09-11 | Wyeth | 7h-pyrrolo[2,3-h]quinazoline compounds, their use as mtor kinase and pi3 kinase inhibitors, and their synthesis |
| JPWO2009128520A1 (en) * | 2008-04-18 | 2011-08-04 | 塩野義製薬株式会社 | Heterocyclic compounds having PI3K inhibitory activity |
| EP2303890A4 (en) * | 2008-06-19 | 2012-04-11 | Progenics Pharm Inc | Phosphatidylinositol 3 kinase inhibitors |
| EP2168583A1 (en) | 2008-09-24 | 2010-03-31 | Bayer Schering Pharma Aktiengesellschaft | Use of substituted 2,3-dihydroimidazo[1,2-c]quinazolines for the treatment of myeloma |
| EP2168582A1 (en) | 2008-09-24 | 2010-03-31 | Bayer Schering Pharma Aktiengesellschaft | Combinations of substituted 2,3-dihydroimidazo[1,2-c]quinazolines |
| US8791131B2 (en) * | 2008-09-30 | 2014-07-29 | Pfizer Inc. | Imidazo[1,5]naphthyridine compounds, their pharmaceutical use and compositions |
| MX2011004957A (en) * | 2008-11-11 | 2011-08-12 | Je Il Pharmaceutical Co Ltd | Novel tricyclic derivative or pharmaceutically acceptable salts thereof, preparation method thereof, and pharmaceutical composition containing the same. |
| EP3427739A1 (en) | 2008-11-13 | 2019-01-16 | Gilead Calistoga LLC | Therapies for hematologic malignancies |
| US9492449B2 (en) | 2008-11-13 | 2016-11-15 | Gilead Calistoga Llc | Therapies for hematologic malignancies |
| US10236078B2 (en) | 2008-11-17 | 2019-03-19 | Veracyte, Inc. | Methods for processing or analyzing a sample of thyroid tissue |
| US9495515B1 (en) | 2009-12-09 | 2016-11-15 | Veracyte, Inc. | Algorithms for disease diagnostics |
| US9090601B2 (en) | 2009-01-30 | 2015-07-28 | Millennium Pharmaceuticals, Inc. | Thiazole derivatives |
| WO2010090716A1 (en) | 2009-01-30 | 2010-08-12 | Millennium Pharmaceuticals, Inc. | Heteroaryls and their use as pi3k inhibitors |
| NZ595307A (en) | 2009-03-24 | 2013-11-29 | Gilead Calistoga Llc | Atropisomers of 2-purinyl-3-tolyl-quinazolinone derivatives and methods of use |
| MX2011011036A (en) | 2009-04-20 | 2012-01-20 | Gilead Calistoga Llc | Methods of treatment for solid tumors. |
| TWI562992B (en) * | 2009-04-30 | 2016-12-21 | Glaxo Group Ltd | Indazole derivative, pharmaceutical composition thereof, and use thereof as inhibitors of kinase activity |
| US8669057B2 (en) | 2009-05-07 | 2014-03-11 | Veracyte, Inc. | Methods and compositions for diagnosis of thyroid conditions |
| EA201270184A1 (en) | 2009-07-21 | 2012-08-30 | ГИЛИЭД КАЛИСТОГА ЭлЭлСи | TREATMENT OF LIVER DISORDERS PI3K INHIBITORS |
| BR112012008385A2 (en) * | 2009-09-09 | 2019-09-24 | Avila Therapeutics Inc | p13 kinase inhibitors and their use. |
| US20130184270A1 (en) | 2010-04-16 | 2013-07-18 | Bayer Intellectual Property Gmbh | Substituted 2,3-dihydroimidazo[1,2-c]quinazoline-containing combinations |
| US9062038B2 (en) | 2010-08-11 | 2015-06-23 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| EA201300420A1 (en) | 2010-10-01 | 2013-09-30 | Байер Интеллектчуал Проперти Гмбх | COMBINATIONS WHICH CONTAIN N SUBSTITUTED N- (2-ARYLAMINO) ARYLSULPHONAMIDE |
| US9675616B2 (en) | 2010-11-11 | 2017-06-13 | Bayer Intellectual Property Gmbh | Arylaminoalcohol-substituted 2,3-dihydroimidazo[1,2-C]quinolines |
| US9730943B2 (en) | 2010-11-11 | 2017-08-15 | Bayer Intellectual Property Gmbh | Alkoxy-substituted 2,3-dihydroimidazo[1,2-C]quinazolines |
| UA113280C2 (en) * | 2010-11-11 | 2017-01-10 | AMINOSPIRT-SUBSTITUTED Derivatives of 2,3-Dihydroimimidase $ 1,2-c] QINAZOLINE, SUITABLE FOR THE TREATMENT OF HYPERPROLIFERATIVE DISORDERS, DISEASES AND DISEASES | |
| JO3733B1 (en) | 2011-04-05 | 2021-01-31 | Bayer Ip Gmbh | Use of 3,2-dihydroimidazo[1,2-C]substituted quinazolines |
| EP2508525A1 (en) | 2011-04-05 | 2012-10-10 | Bayer Pharma Aktiengesellschaft | Substituted 2,3-dihydroimidazo[1,2-c]quinazoline salts |
| ES2848273T3 (en) | 2012-03-05 | 2021-08-06 | Gilead Calistoga Llc | Polymorphic forms of (S) -2- (1- (9H-purin-6-ylamino) propyl) -5-fluoro-3-phenylquinazoline-4 (3H) -one |
| US10526655B2 (en) | 2013-03-14 | 2020-01-07 | Veracyte, Inc. | Methods for evaluating COPD status |
| US11976329B2 (en) | 2013-03-15 | 2024-05-07 | Veracyte, Inc. | Methods and systems for detecting usual interstitial pneumonia |
| CN105339001A (en) | 2013-03-15 | 2016-02-17 | 基因泰克公司 | Methods of treating cancer and preventing cancer drug resistance |
| UA122822C2 (en) | 2013-04-08 | 2021-01-06 | Байєр Фарма Акцієнгезелльшафт | APPLICATION OF SUBSTITUTED 2,3-DIHYDROIMIDAZO[1,2-c]QUINAZOLINES FOR THE TREATMENT OF LYMPHOMA |
| SG10201707002VA (en) | 2013-05-01 | 2017-10-30 | Hoffmann La Roche | Biheteroaryl compounds and uses thereof |
| WO2015027431A1 (en) | 2013-08-29 | 2015-03-05 | Merck Sharp & Dohme Corp. | 2,2-difluorodioxolo a2a receptor antagonists |
| ES2752552T3 (en) | 2013-12-20 | 2020-04-06 | Gilead Calistoga Llc | Process methods for phosphatidylinositol 3-kinase inhibitors |
| EP3083623A1 (en) | 2013-12-20 | 2016-10-26 | Gilead Calistoga LLC | Polymorphic forms of a hydrochloride salt of (s) -2-(9h-purin-6-ylamino) propyl) -5-fluoro-3-phenylquinazolin-4 (3h) -one |
| NZ726360A (en) | 2014-06-13 | 2018-04-27 | Gilead Sciences Inc | Phosphatidylinositol 3-kinase inhibitors |
| US12297505B2 (en) | 2014-07-14 | 2025-05-13 | Veracyte, Inc. | Algorithms for disease diagnostics |
| US20170335396A1 (en) | 2014-11-05 | 2017-11-23 | Veracyte, Inc. | Systems and methods of diagnosing idiopathic pulmonary fibrosis on transbronchial biopsies using machine learning and high dimensional transcriptional data |
| EP3018131A1 (en) | 2014-11-07 | 2016-05-11 | Bayer Pharma Aktiengesellschaft | Synthesis of copanlisib and its dihydrochloride salt |
| EP3018127A1 (en) | 2014-11-07 | 2016-05-11 | Bayer Pharma Aktiengesellschaft | Synthesis of copanlisib and its dihydrochloride salt |
| EA201791974A1 (en) | 2015-03-09 | 2018-05-31 | Байер Фарма Акциенгезельшафт | COMBINATIONS CONTAINING SUBSTITUTE 2,3-DIHYDROIMIDAZO [1,2-С] HINAZOLIN |
| CN105130998B (en) * | 2015-09-25 | 2017-07-28 | 苏州立新制药有限公司 | Ku Pannixi preparation method |
| CN105130997B (en) * | 2015-09-25 | 2017-12-05 | 苏州明锐医药科技有限公司 | A kind of Ku Pannixi preparation method |
| CA3016584A1 (en) | 2016-03-08 | 2017-09-14 | Bayer Pharma Aktiengesellschaft | 2-amino-n-[7-methoxy-2,3-dihydroimidazo-[1,2-c]quinazolin-5-yl]pyrimidine-5-carboxamides |
| EP3219329A1 (en) | 2016-03-17 | 2017-09-20 | Bayer Pharma Aktiengesellschaft | Combinations of copanlisib |
| WO2018009915A1 (en) | 2016-07-08 | 2018-01-11 | Trustees Of Boston University | Gene expression-based biomarker for the detection and monitoring of bronchial premalignant lesions |
| JP2019532922A (en) | 2016-09-23 | 2019-11-14 | バイエル ファーマ アクチエンゲゼルシャフト | PI3K-inhibitor combinations |
| WO2018112176A1 (en) | 2016-12-14 | 2018-06-21 | Tarveda Therapeutics, Inc. | Hsp90-targeting conjugates and formulations thereof |
| CA3054249A1 (en) | 2017-02-24 | 2018-08-30 | Bayer Pharma Aktiengesellschaft | Combinations of copanlisib with anti-pd-1 antibody |
| CA3068324A1 (en) | 2017-06-28 | 2019-01-03 | Bayer Consumer Care Ag | Combination of a pi3k-inhibitor with an androgen receptor antagonist |
| EP3498266A1 (en) | 2017-12-15 | 2019-06-19 | Bayer Consumer Care AG | Formulations of copanlisib |
| JP2020533292A (en) | 2017-09-08 | 2020-11-19 | バイエル・コンシューマー・ケア・アクチェンゲゼルシャフトＢａｙｅｒ Ｃｏｎｓｕｍｅｒ Ｃａｒｅ ＡＧ | Copanricib formulation |
| CA3076202A1 (en) * | 2017-09-20 | 2019-03-28 | Abm Therapeutics Corporation | Cyclic iminopyrimidine derivatives as kinase inhibitors |
| US11351156B2 (en) | 2017-10-13 | 2022-06-07 | Inserm | Combination treatment of pancreatic cancer |
| EP3713963A1 (en) | 2017-11-23 | 2020-09-30 | INSERM (Institut National de la Santé et de la Recherche Médicale) | A new marker for predicting the sensitivity to pi3k inhibitors |
| WO2019105734A1 (en) | 2017-11-28 | 2019-06-06 | Bayer Consumer Care Ag | Combinations of copanlisib |
| WO2019105835A1 (en) | 2017-11-29 | 2019-06-06 | Bayer Consumer Care Ag | Combinations of copanlisib and anetumab ravtansine |
| WO2019197269A1 (en) | 2018-04-11 | 2019-10-17 | Bayer Aktiengesellschaft | Combinations of copanlisib with triazolone derivatives and their use in the treatment of cancer |
| CN112789279B (en) * | 2018-07-27 | 2023-09-29 | 上海翰森生物医药科技有限公司 | Inhibitor containing tricyclic derivatives, preparation method and application thereof |
| CN109053554B (en) * | 2018-08-01 | 2020-07-28 | 江苏八巨药业有限公司 | Method for synthesizing 3-acetylpyridine by using catalyst |
| CA3110754A1 (en) | 2018-08-28 | 2020-03-05 | Bayer As | Combination of pi3k-inhibitors and targeted thorium conjugates |
| EP3866805A1 (en) | 2018-10-16 | 2021-08-25 | Bayer Aktiengesellschaft | Combination of atr kinase inhibitors with 2,3-dihydroimidazo[1,2-c]quinazoline compounds |
| MX2021004775A (en) | 2018-11-05 | 2021-06-08 | Iovance Biotherapeutics Inc | EXPANSION OF TUMOR-INFILTRATING LYMPHOCYTES (TILS) USING INHIBITORS OF THE PROTEIN KINASE B PATHWAY (AKT). |
| AU2019407426A1 (en) | 2018-12-21 | 2021-07-22 | Daiichi Sankyo Company, Limited | Combination of antibody-drug conjugate and kinase inhibitor |
| WO2020164997A1 (en) | 2019-02-12 | 2020-08-20 | Bayer Aktiengesellschaft | Combination of pi3k-inhibitors |
| CN114621236B (en) * | 2022-04-25 | 2024-06-18 | 河南湾流生物科技有限公司 | Preparation method of quinoline feed additive |
| WO2025087879A2 (en) | 2023-10-23 | 2025-05-01 | Institut National de la Santé et de la Recherche Médicale | Suppressing the pi3kgamma/akt signalling pathway for the treatment of acute myeloid leukemia |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3644354A (en) * | 1968-09-16 | 1972-02-22 | Sandoz Ag | 5-substituted-2 3-dihydroimidazo(1 2-c)quinazolines |
| US4287341A (en) | 1979-11-01 | 1981-09-01 | Pfizer Inc. | Alkoxy-substituted-6-chloro-quinazoline-2,4-diones |
| NZ234186A (en) * | 1989-07-07 | 1991-10-25 | Janssen Pharmaceutica Nv | Imidazo quinazolin-one derivatives and pharmaceutical compositions |
| CN1033644C (en) * | 1993-01-02 | 1996-12-25 | 瑞安大药厂股份有限公司 | 3-substituted methyl-2,3-dihydroimidazo[1,2-c]quinazoline derivatives, their preparation and use |
| CA2197205A1 (en) | 1994-08-12 | 1996-02-22 | Reid W. Vonborstel | Methods for treating sepsis or inflammatory diseases with oxypurine nucleosides |
| EP0885192B8 (en) * | 1996-01-29 | 2012-05-16 | The United States of America, Represented by the Secretary, Department of Health and Human Services | Dihydropyridine-, pyridine-, benzopyran- one- and triazoloquinazoline derivative, their preparation and their use as adenosine receptor antagonists |
| US5932584A (en) * | 1997-05-06 | 1999-08-03 | National Science Council | Optically active 2,3-dihydroimidazo(1,2-C) quinazoline derivatives, the preparation and antihypertensive use thereof |
| CA2406278C (en) | 2000-04-25 | 2012-06-05 | Icos Corporation | Inhibitors of human phosphatidyl-inositol 3-kinase delta |
| JP3649395B2 (en) * | 2000-04-27 | 2005-05-18 | 山之内製薬株式会社 | Fused heteroaryl derivatives |
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